Plural Ring Sulfurs In The Five-membered Hetero Ring Patents (Class 548/123)
  • Patent number: 8658650
    Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: February 25, 2014
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
  • Patent number: 8343913
    Abstract: A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: January 1, 2013
    Assignee: Whitehead Institute for Biomedical Research
    Inventors: Leah Cowen, Susan L. Lindquist
  • Publication number: 20120277185
    Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.
    Type: Application
    Filed: July 10, 2010
    Publication date: November 1, 2012
    Applicant: BAYER CROPSCIENDE AG
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Patent number: 8227504
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: July 24, 2012
    Assignee: Sanofi
    Inventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
  • Publication number: 20110319429
    Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.
    Type: Application
    Filed: January 28, 2010
    Publication date: December 29, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
  • Patent number: 8058448
    Abstract: The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: November 15, 2011
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Michael E. Jung, Kallanthottathil G. Rajeev, Rajendra K. Pandey, Gang Wang
  • Patent number: 8017558
    Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Grant
    Filed: December 5, 2006
    Date of Patent: September 13, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Patent number: 7989635
    Abstract: Methods for preparing an ammonium salt and a lithium salt of a fluorinated bis-sulfonylimide by a practical and efficient method with a high yield with a small number of steps. Further, a high purity ammonium salt of a fluorinated bis-sulfonylimide useful for the method for producing a lithium salt is provided. A method for producing a purified particulate solid (II) of a salt represented by the formula (1), which comprises suspending a particulate solid (I) of a salt represented by the formula (1) in a solvent comprising an etheric oxygen atom-containing compound, and separating the solvent by filtration: [HNR3]+[Q1-SO2—N—SO2-Q2]???(1) wherein each of R's which may be the same or different, is a hydrogen atom or a C1-10 alkyl group, and each of Q1 and Q2 which are independent of each other, is a monovalent fluoroorganic group, or Q1 and Q2 together form a bivalent fluoroorganic group.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: August 2, 2011
    Assignee: Asahi Glass Company, Limited
    Inventor: Masao Iwaya
  • Publication number: 20110137021
    Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones, 5-phenyl-3H-1,2,4-dithiazole-3-thiones, and derivatives thereof as novel, efficient sulfur-transfer reagents is disclosed. Sulfur transfer from these reagents to compounds containing a P(III) atom (e.g., triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite), was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 9, 2011
    Inventor: Andrei P. Guzaev
  • Patent number: 7951523
    Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Using an alkaline soluble polymer, a crosslinking agent, and a solvent capable of dissolving them as at least constituent component, a composition is prepared and a protective film is formed on the surface of the resist film to be used, using the composition.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: May 31, 2011
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Keita Ishizuka, Kotaro Endo, Tomovuki Hiranoa
  • Patent number: 7947685
    Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: May 24, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Patent number: 7923142
    Abstract: There are provided a novel onium salt and a method for optimizing the interface of a negative electrode by the use of the novel onium salt and/or a conventional onium salt. Such a method is characterized in that an electrolyte comprising novel 2,2,2-trifluoro-N-(trifluoromethanesulfonyl)acetamide•tetraethyl ammonium salt is made to intervene between a negative electrode and a positive electrode in an electrochemical device having the constitution: a negative electrode|an electrolyte|a positive electrode, thereby constructing an electrode structure in the electrochemical device, and applying a voltage between the negative electrode and the positive electrode so as for the negative electrode to have a potential of ?1 V to ?5 V in terms of the potential relative to a reference electrode of I?/I3?, thereby forming a passive-state layer comprising a decomposition product of the above electrolyte or salt on the surface of the above negative electrode.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: April 12, 2011
    Assignees: Tokuyama Corporation, National Institute of Advanced Industrial Science and Technology
    Inventors: Tomonori Matsunaga, Takeo Kawahara, Hajime Matsumoto
  • Patent number: 7910745
    Abstract: It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.
    Type: Grant
    Filed: May 15, 2006
    Date of Patent: March 22, 2011
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Masahito Toyama, Fumie Kurosaki, Akio Hayashi, Osamu Ito
  • Patent number: 7879529
    Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Furthermore, it is possible to apply a high refractive index liquid immersion medium, used in combination with the high refractive index liquid immersion medium, thus making it possible to further improve pattern accuracy. Using a composition comprising an acrylic resin component having characteristics which have substantially no compatibility with a liquid in which a resist film is immersed, particularly water, and are also soluble in alkaline, a protective film is formed on the surface of a resist film used.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: February 1, 2011
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Kotaro Endo, Masaaki Yoshida, Keita Ishizuka
  • Publication number: 20100256384
    Abstract: Methods for preparing an ammonium salt and a lithium salt of a fluorinated bis-sulfonylimide by a practical and efficient method with a high yield with a small number of steps. Further, a high purity ammonium salt of a fluorinated bis-sulfonylimide useful for the method for producing a lithium salt is provided. A method for producing a purified particulate solid (II) of a salt represented by the formula (1), which comprises suspending a particulate solid (I) of a salt represented by the formula (1) in a solvent comprising an etheric oxygen atom-containing compound, and separating the solvent by filtration: [HNR3]+[Q1-SO2—N—SO2-Q2]???(1) wherein each of R? s which may be the same or different, is a hydrogen atom or a C1-10 alkyl group, and each of Q1 and Q2 which are independent of each other, is a monovalent fluoroorganic group, or Q1 and Q2 together form a bivalent fluoroorganic group.
    Type: Application
    Filed: June 21, 2010
    Publication date: October 7, 2010
    Applicant: ASAHI GLASS COMPANY, LIMITED
    Inventor: Masao IWAYA
  • Patent number: 7786293
    Abstract: The present invention provides a process for the sulfurization of phosphorus-containing compounds. More particularly, the process involves contacting the compound to be sulfurized with a sulfur transfer reagent as defined hereinbefore in a solvent or a mixture of solvents.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: August 31, 2010
    Assignee: Novartis AG
    Inventors: Pierre Martin, Francois Jean Charles Natt
  • Publication number: 20100137609
    Abstract: Methods for preparing an ammonium salt and a lithium salt of a fluorinated bis-sulfonylimide by a practical and efficient method with a high yield with a small number of steps. Further, a high purity ammonium salt of a fluorinated bis-sulfonylimide useful for the method for producing a lithium salt is provided. A method for producing a purified particulate solid (II) of a salt represented by the formula (1), which comprises suspending a particulate solid (I) of a salt represented by the formula (1) in a solvent comprising an etheric oxygen atom-containing compound, and separating the solvent by filtration: [HNR3]+[Q1-SO2—N—SO2-Q2]???(1) wherein each of R's which may be the same or different, is a hydrogen atom or a C1-10 alkyl group, and each of Q1 and Q2 which are independent of each other, is a monovalent fluoroorganic group, or Q1 and Q2 together form a bivalent fluoroorganic group.
    Type: Application
    Filed: February 4, 2010
    Publication date: June 3, 2010
    Applicant: ASAHI GLASS COMPANY, LIMITED
    Inventor: Masao IWAYA
  • Patent number: 7723528
    Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones as novel, efficient sulfur-transfer reagents is disclosed. The sulfur transfer from these reagents to compounds containing P(III) atom, triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite, was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: May 25, 2010
    Assignee: AM Chemicals LLC
    Inventor: Andrei P. Guzaev
  • Patent number: 7678789
    Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: February 9, 2006
    Date of Patent: March 16, 2010
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Roelof W. Feenstra, Hiskias G. Keizer, Maria L. Pras-Raves, Bernard J Van Vliet, Gustaaf J. M. Van Scharrenburg
  • Publication number: 20090306358
    Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones as novel, efficient sulfur-transfer reagents is disclosed. The sulfur transfer from these reagents to compounds containing P(III) atom, triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite, was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.
    Type: Application
    Filed: June 5, 2008
    Publication date: December 10, 2009
    Inventor: Andrei P. Guzaev
  • Patent number: 7612059
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: November 3, 2009
    Assignee: Vicuron Pharmaceuticals, Inc.
    Inventors: Jeffrey Jacobs, Rakesh K Patel, Jason G Lewis, Dinesh V Patel, Zhengyu Yuan
  • Patent number: 7579465
    Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: August 25, 2009
    Assignee: Biota Scientific Managment Pty. Ltd.
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Publication number: 20090187027
    Abstract: The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups.
    Type: Application
    Filed: January 9, 2009
    Publication date: July 23, 2009
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah MANOHARAN, Michael E. JUNG, Kallanthottathil G. RAJEEV, Rajendra K. PANDEY, Gang WANG
  • Patent number: 7553964
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: June 1, 2006
    Date of Patent: June 30, 2009
    Assignee: Abbott Laboratories
    Inventors: Huaqing Liu, Kathryn J. Hancock, legal representative, Marlon D. Cowart, Arthur A. Hancock
  • Patent number: 7348017
    Abstract: A dithiazole compound or a salt thereof is disclosed. The compound inhibits matrix metalloprotease (MMPs) activity and can be used in pharmaceutical and cosmetic compositions for the treatment of skin conditions.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: March 25, 2008
    Assignee: Shiseido Co., Ltd.
    Inventors: Takuya Hiruma, Koji Kobayashi, Shinji Inomata
  • Patent number: 7297797
    Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: November 20, 2007
    Assignee: Bayer CropScience AG
    Inventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
  • Patent number: 7198651
    Abstract: The present invention relates to a method to achieve a reversible change of the colour of hair dyed with an azo dye wherein the change of the colour can be effected by, for example, the salonist or the consumer in a simple manner. The colour of the hair thus dyed may be changed simply by treating the dyed hair with an acid treatment composition at any time after the first dyeing treatment. If desired by the consumer, the colour may be returned to substantially the original post dye colour by treating the hair further with an alkaline treatment composition.
    Type: Grant
    Filed: November 26, 2004
    Date of Patent: April 3, 2007
    Assignees: Kao Corporation, Fuji Photo Film Co., Ltd.
    Inventors: Dominic Pratt, Masayoshi Nojiri, Toshio Kawagishi
  • Patent number: 7105556
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Patent number: 7098325
    Abstract: The invention relates to a process for the sulfurization of phosphorus-containing compounds which comprises contacting the phosphorus compound to be sulfurized with a sulfur transfer reagent of formula (I) wherein R1 is aryl which can be substituted by halo, (C1–C6) alkyl or (C1-C6) alkoxy, and R2 is (C1–C6) alkyl, which could also form a cyclic ring together with R1, in a solvent or a mixture of solvents.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: August 29, 2006
    Inventors: Pierre Martin, Francois J Natt
  • Patent number: 7087621
    Abstract: The present invention provides compounds of formula I or a pharmaceutically acceptable salt, solvate, prodrug or isomer thereof and compounds of the formula or a pharmaceutically acceptable salt, solvate, prodrug or isomer thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: September 1, 2004
    Date of Patent: August 8, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiaopeng Sang, Xuhua Karen Du, John F. Kadow
  • Patent number: 6987104
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6927215
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 2 to 10, n represents 0, 1 or 2. y represents unsubstituted or substituted methylene and p represents 1, 2 or 3, and to processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: August 9, 2005
    Assignee: Bayer Cropscience AG
    Inventors: Udo Kraatz, Bernd Gallenkamp, Heiko Rieck, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Peter Lösel, Andreas Turberg, Olaf Hansen, Achim Harder
  • Patent number: 6872833
    Abstract: The present invention relates to compounds of the general formula I wherein R1, R2, R?, R?, n, m and o are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of general formula I are adenosine receptor ligands with a good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds have useful pharmacological activities.
    Type: Grant
    Filed: March 30, 2004
    Date of Patent: March 29, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roger David Norcross
  • Patent number: 6863698
    Abstract: A method for coloring Keratin-containing fibers which comprises applying a composition containing a compound of formula A—CH?B—CH?A???(I).
    Type: Grant
    Filed: June 24, 2002
    Date of Patent: March 8, 2005
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Horst Hoeffkes, David Rose, Bernd Meinigke
  • Publication number: 20040236111
    Abstract: A dithiazole compound or a salt thereof expressed by formula (I): 1
    Type: Application
    Filed: February 23, 2004
    Publication date: November 25, 2004
    Inventors: Takuya Hiruma, Koji Kobayashi, Shinji Inomata
  • Publication number: 20040138470
    Abstract: Novel chiral diphosphines (R) or (S), and their use as optically active ligand for preparing diphosphino-metallic complexes, and the diphosphino-metallic complexes containing said chiral diphosphines (R) or (S), and the use of the diphosphino-metallic complexes as catalyst in asymmetric catalysis of unsaturated compounds bearing functional groups.
    Type: Application
    Filed: November 20, 2003
    Publication date: July 15, 2004
    Inventors: Jean-Pierre Genet, Angela Marinetti, Guillaume Michaud, Michel Bulliard
  • Publication number: 20040127525
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: January 30, 2004
    Publication date: July 1, 2004
    Inventors: Udo Kraatz, Bernd Gallenkamp, Heiko Rieck, Albrecht Marhold, Peter Wolfrum, Wolfram andersch, Christoph Erdelen, Peter Losel, Andreas Turberg, Olaf Hansen, Achim Harder
  • Patent number: 6610707
    Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: August 26, 2003
    Assignee: Pfizer Inc.
    Inventors: David John Bull, Robert John Maguire, Michael John Palmer, Martin James Wythes
  • Patent number: 6608175
    Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: August 19, 2003
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 6589914
    Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: July 8, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
  • Patent number: 6583289
    Abstract: The present invention provides a new class of materials effective as curatives for anaerobic adhesive compositions. The addition of these materials into anaerobic adhesives as a replacement for conventional curatives, such as APH, surprisingly provides at least comparable cure speeds and physical properties for the reaction products formed therefrom.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: June 24, 2003
    Assignee: Loctite (R&D) Limited
    Inventors: Ciaran B. McArdle, Rory B. Barnes
  • Publication number: 20030097003
    Abstract: An electron accepting monomer having the formula: 1
    Type: Application
    Filed: October 28, 2002
    Publication date: May 22, 2003
    Inventors: Geoffrey A. Lindsay, Richard A. Hollins, Mathew C. Davis, Andrew P. Chafin
  • Patent number: 6531496
    Abstract: The invention relates to new O-aryldithiazole dioxides, to two processes for their preparation, and to their use as pesticides in crop protection and in the protection of materials.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: March 11, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann Uhr, Christiane Boie, Heiko Rieck, Bernd-Wieland Krüger, Ulrich Heinemann, Robert Markert, Martin Vaupel, Martin Kugler, Klaus Stenzel, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Peter Lösel, Shinichi Narabu
  • Patent number: 6525086
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: February 25, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Publication number: 20030004193
    Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.
    Type: Application
    Filed: July 23, 2002
    Publication date: January 2, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
  • Patent number: 6417209
    Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: July 9, 2002
    Assignee: GPI Nil Holdings, Inc.
    Inventors: Gregory S. Hamilton, Jia-He Li
  • Publication number: 20020052510
    Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.
    Type: Application
    Filed: December 3, 1998
    Publication date: May 2, 2002
    Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
  • Patent number: 6331537
    Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: December 18, 2001
    Assignee: GPI Nil Holdings, Inc.
    Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
  • Patent number: 6316476
    Abstract: The invention is drawn to novel antibiotics, XENORXIDES of formula shown below, wherein R1, R2=hydrogen, substituted or unsubstituted alkyl, cycloalkyl, acyl, aryl, aralkyl, or heterocyclyl group; R3=hydrogen, alkyl cycloalkyl, aralkyl or aryl group, produced by bacterial symbiont Xenorhabdus bovienii and/or other Xenorhabdus species, and/or by oxidation of the corresponding dithiolopyrrolone derivatives with oxygen and Xenorhabdus species, and/or its cell-free filtrate, the additional salts thereof, the compositions thereof and their use as medicaments and/or agrochemicals, particularly in the treatment of infectious diseases involving microorganisms susceptible to them, including drug-resistant Staphylococcus.
    Type: Grant
    Filed: July 23, 1996
    Date of Patent: November 13, 2001
    Assignee: Welichem Biotech Inc.
    Inventors: John M. Webster, Jianxiong Li, Genhui Chen
  • Patent number: 6313164
    Abstract: Compounds of the formula (I): wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of the formula —N(R2)CO—, —N(R2)CS—, —N(R2)SO2—, —CON(R2)N(R3)CO—, —CON(R2)CO—, —CON(R2)CS—, —CON(R2)SO2—, —O—CO—, —ON(R2)CO—, —ON(R2)SO2—, —O—CON(R2)N(R3)CO—, —O—CON(R2)CO—, —O—CON(R2)SO2—, —CO—O—, —CO—CO—, —CO—CON(R2)N(R3)CO—, —CO—CON(R2)CO—, —CO—CON(R2)SO2—, —N(R2)O—, —N(R2)COCO—, —N(R2)N(R3)CO—, —N(R2)N(R3)SO2—, —N(R2)CON(R3)N(R4)CO—, —N(R2)CON(R3)CO—, —N(R2)CON(R3)SO2&mdas
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: November 6, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Takashi Fujita, Tomihisa Yokoyama